Assay Detail
Binding
CHEMBL4737389
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDK (unknown origin) using RYHGHSMSDP as substrate after 30 mins by Kinase-Glo luminescent assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 6.56 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1231132 | — | — | 1 | 7.28 |
| CHEMBL4746836 | — | — | 1 | 7.05 |
| CHEMBL4278654 | — | — | 1 | 6.48 |
| CHEMBL4764301 | — | — | 1 | 6.47 |
| CHEMBL4782703 | — | — | 1 | 6.26 |
| CHEMBL4741315 | — | — | 1 | 5.83 |
| CHEMBL3560171 | — | — | 1 | - |
| CHEMBL306823 | SODIUM DICHLOROACETATE | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1231132 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4746836 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4278654 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4764301 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4782703 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4741315 | — | EC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL3560171 | — | EC50 | > | 80000.0 | nM | - |
| CHEMBL306823 | SODIUM DICHLOROACETATE | EC50 | > | 100000000.0 | nM | - |